The rapidly expanding range of neuronal benzodiazepine receptor ligands

Cr, Gardner; Wr, Tully; Cj, Hedgecock

doi:10.1016/0301-0082(93)90047-v

Cited by 83 publications

(33 citation statements)

References 203 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…All these drugs mediate their CNS effects through interaction with the GABA A receptor complex by potentiation of inhibitory activities of GABA [for reviews, see [12][13][14]. While most of the compounds are synthetic [13,15,16], a range of plant-derived compounds interacted with GABA A receptor complex with diverse properties [for reviews, see 3,17].…”

Section: Discussionmentioning

confidence: 99%

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

Wang²,

Nielsen³

2001

Pharmacology

View full text Add to dashboard Cite

Honokiol and magnolol have been identified as modulators of the GABA_A receptors in vitro. Our previous study suggested a possible selectivity of honokiol and magnolol on GABA_Areceptor subtypes. This possibility was examined in the current study by ³H-muscimol and ³H-flunitrazepam binding assays on various rat brain membrane preparations and human recombinant GABA_A receptor subunit combinations expressed by the Sf-9/baculovirus system. Generally, honokiol and magnolol have a similar enhancing effect on ³H-muscimol binding to various membrane preparations in nonsaturation binding assays. Honokiol and magnolol preferentially increased ³H-muscimol binding to hippocampus compared to cortex and cerebellum (with a maximum enhancement of 400% of control). As for subunit combinations, honokiol and magnolol have a more potent enhancing effect on α₂ subunit containing combinations (with a maximum enhancement of 400–450% of control). This action was independent of the γ subunit. In saturation binding assays, magnolol affected either the number of binding sites (ca. 4-fold on α₂ containing combinations) or the binding affinity (on α₁ containing combinations) of ³H-muscimol binding to various GABA_A receptor subunit combinations. In contrast, honokiol increased only binding sites on α₂β₃γ_2s and α₂β₃ combinations, but both the number of binding sites and the binding affinity on α₁β₂γ_2S and α₁β₂ combinations. These results indicate that honokiol and magnolol have some selectivity on different GABA_A receptor subtypes. The property of interacting with GABA_A receptors and their selectivity could be responsible for the reported in vivo effects of these two compounds.

show abstract

Section: Discussionmentioning

confidence: 99%

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

Wang²,

Nielsen³

2001

Pharmacology

View full text Add to dashboard Cite

show abstract

“…Benzodiazepine binding site ligands are classified as positive allosteric modulators, antagonists, or negative allosteric modulators according to their spectrum of intrinsic efficacy towards the GABA A receptor (Gardner et al, 1993). Positive allosteric modulators increase the frequency of chloride channel openings without altering the channel conductance or duration of opening.…”

Section: Discussionmentioning

confidence: 99%

The Scutellaria Flavone, Oroxylin A, Improves Attention-Deficit/Hyperactivity Disorder Related Behaviors in Spontaneously Hypertensive Rats

Yoon¹,

Chun²,

Lee³

et al. 2008

Biomolecules and Therapeutics

View full text Add to dashboard Cite

− Oroxylin A is a flavonoid isolated from Scutellaria baicalensis, which is one of the most important medicinal herbs in traditional Korean medicine. In this study, we investigated the psychopharmacological activities of oroxylin A using the open field, rota-rod, balanced wire and plus-maze tests in Spontaneously Hypertensive Rats (SHR) and Wistar Kyoto Rats (WKY). Oroxylin A reduced hyperactivity in SHR (ADHD animal model) although it tended to increase locomotor activity in WKY. Methylphenidate did not reduce hyperactivity. Oroxylin A alleviated impulsive behaviors such as rearing, the percentage of moving time to the central area and the tendency to move into an unstable condition (open area in elevated plus-maze). Methylphenidate also reduced the percentage of staying time in the central area and the tendency to move into an unstable condition. Both oroxylin A and methylphenidate enhanced motor attention in SHR and WKY. Oroxylin A antagonized the muscimol (GABA A receptor agonist)-induced Cl -current and its action was similar to that of bicuculline (GABA A receptor antagonist). The effects of oroxylin A may be caused by the antagonism at the GABA A receptor. Thus, oroxylin A may be a candidate of drug for treatment of ADHD.

show abstract

“…Anxiety disorders present in a number of forms, although probably all share a number of common neurological circuits (Beck, 1988). Benzodiazepines have been used for the treatment of several forms of anxiety although these compounds have well-known their side-effects such as sedation, muscle relaxation, amnesia and drug dependence (Gardner et al, 1993). So, many researchers have been evaluated new compounds with less undesirable effects from herbs.…”

Section: Introductionmentioning

confidence: 99%

Anxiolytic-Like Effects of Cyclopeptide Fraction Alkaloids of Zizyphi Spinosi Semen: Possible Involvement of GABA_AReceptors

Han¹,

An²,

Eun³

et al. 2008

Biomolecules and Therapeutics

View full text Add to dashboard Cite

However, CFAZ has no effect on the locomotor activity, while diazepam (2.0 mg/kg, p.o.) significantly reduced locomotor activity. CFAZ did not influence the grip force in the grip strength meter test, either. From the molecular experiments, CFAZ increased chloride influx in cultured cerebellar granule cells. In addition, GABA A receptors γ-subunit were over-expressed by CFAZ in cultured cerebellar granule cells. It is concluded that CFAZ may have anxiolytic-like effects, and these effects may be mediated by GABA A receptors.

show abstract

The rapidly expanding range of neuronal benzodiazepine receptor ligands

Cited by 83 publications

References 203 publications

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

The Scutellaria Flavone, Oroxylin A, Improves Attention-Deficit/Hyperactivity Disorder Related Behaviors in Spontaneously Hypertensive Rats

Anxiolytic-Like Effects of Cyclopeptide Fraction Alkaloids of Zizyphi Spinosi Semen: Possible Involvement of GABA_AReceptors

Contact Info

Product

Resources

About

The rapidly expanding range of neuronal benzodiazepine receptor ligands

Cited by 83 publications

References 203 publications

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

Honokiol and Magnolol Selectively Interact with GABA<sub>A</sub> Receptor Subtypes in vitro

The Scutellaria Flavone, Oroxylin A, Improves Attention-Deficit/Hyperactivity Disorder Related Behaviors in Spontaneously Hypertensive Rats

Anxiolytic-Like Effects of Cyclopeptide Fraction Alkaloids of Zizyphi Spinosi Semen: Possible Involvement of GABAAReceptors

Contact Info

Product

Resources

About

Anxiolytic-Like Effects of Cyclopeptide Fraction Alkaloids of Zizyphi Spinosi Semen: Possible Involvement of GABA_AReceptors